Patent classifications
C07D211/26
ENZYME-CLEAVABLE METHADONE PRODRUGS AND METHODS OF USE THEREOF
The present disclosure provides methadone prodrugs, pharmaceutical compositions, and their methods of use, where the pharmaceutical compositions comprise a methadone prodrug that provides enzymatically-controlled release of methadone, and an optional enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of methadone from the prodrug so as to attenuate enzymatic cleavage of the prodrug.
NOVEL SMALL MOLECULE INHIBITORS OF TEAD TRANSCRIPTION FACTORS
The present disclosure compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the TEAD transcription factor, and are useful in the treatment of diseases related to the activity of TEAD transcription factor including, e.g., cancer and other diseases.
FURIN INHIBITORS
This invention relates to novel compounds according to Formula (I) which are inhibitors of furin, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of fibrotic diseases, including pulmonary fibrosis, renal fibrosis, liver fibrosis, skin fibrosis, ocular fibrosis, cardiac fibrosis, and other miscellaneous fibrotic conditions. The disclosed compounds may also be useful for treating other furin-mediated conditions, including but not limited to, hypertension, cancer, infectious diseases, and genetic disorders (e.g., cystic fibrosis (CF)), and neurodegenerative disorders.
##STR00001##
FURIN INHIBITORS
This invention relates to novel compounds according to Formula (I) which are inhibitors of furin, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of fibrotic diseases, including pulmonary fibrosis, renal fibrosis, liver fibrosis, skin fibrosis, ocular fibrosis, cardiac fibrosis, and other miscellaneous fibrotic conditions. The disclosed compounds may also be useful for treating other furin-mediated conditions, including but not limited to, hypertension, cancer, infectious diseases, and genetic disorders (e.g., cystic fibrosis (CF)), and neurodegenerative disorders.
##STR00001##
TRPML MODULATORS
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
COMPOUND FOR TREATING ALZHEIMERS DISEASE
Provided in the present invention are a compound as shown in formula I, various crystal forms thereof, a hydrate, a solvate or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition. The compound of the present invention can effectively treat Alzheimer's disease or Down's syndrome, especially cognitive function impairment caused by Alzheimer's disease or Down's syndrome. Also disclosed in the present invention is use of a ubiquitin specific protease USP25 encoded and expressed by chromosome 21 for preventing, treating or ameliorating Alzheimer's disease or Down's syndrome.
##STR00001##
COMPOUND FOR TREATING ALZHEIMERS DISEASE
Provided in the present invention are a compound as shown in formula I, various crystal forms thereof, a hydrate, a solvate or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition. The compound of the present invention can effectively treat Alzheimer's disease or Down's syndrome, especially cognitive function impairment caused by Alzheimer's disease or Down's syndrome. Also disclosed in the present invention is use of a ubiquitin specific protease USP25 encoded and expressed by chromosome 21 for preventing, treating or ameliorating Alzheimer's disease or Down's syndrome.
##STR00001##
SMALL MOLECULE AGONISTS OF MUCOLIPIN 1 AND USES THEREOF
This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a phenyl-sulfonic amide (or similar) structure which function as agonists of mucolipin 1 (ML1), and their use as therapeutics for the treatment of Duchenne muscular dystrophy (DMD) and related disorders.
SMALL MOLECULE AGONISTS OF MUCOLIPIN 1 AND USES THEREOF
This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a phenyl-sulfonic amide (or similar) structure which function as agonists of mucolipin 1 (ML1), and their use as therapeutics for the treatment of Duchenne muscular dystrophy (DMD) and related disorders.
ARYLMETHYLENE HETEROCYCLIC COMPOUNDS AS KV1.3 POTASSIUM SHAKER CHANNEL BLOCKERS
A compound of Formula (I) or a pharmaceutically acceptable salt thereof is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.
##STR00001##